Products
Prasugrel is commercially available in the form of film-coated tablets (Efient). It was approved in many countries, in the EU and in the US in 2009. Generic versions were registered in 2019.
Structure and properties
Prasugrel (C20H20FNO3S, Mr = 373.4 g/mol) belongs to the group of thienopyridines and exists as a hydrochloride as a white powder that is sparingly soluble in water at a neutral pH. In generic drugs, it is also present as hydrobromide. Prasugrel is a prodrug that is metabolized first by esterases and then by CYP450 isozymes. CYP3A and CYP2B6 are primarily involved in the formation of the active metabolite.
Effects
Prasugrel (ATC B01AC22) has antiplatelet and antithrombotic properties. The effects are due to irreversible antagonism of the active metabolite at the P2Y12 ADP receptor.
Indications
In combination with acetylsalicylic acid for prevention of atherothrombotic events in patients undergoing primary or delayed percutaneous coronary intervention, acute coronary syndrome, or ST-segment elevation myocardial infarction.
Dosage
According to the drug label. Prasugrel is usually taken once daily, independent of meals. Treatment is started with a higher initial dose.
Contraindications
- Hypersensitivity
- Acute, pathological bleeding
- History of stroke or transient ischemic attack (TIA).
- Severe liver dysfunction
Full precautions can be found in the drug label.
Interactions
Prasugrel is metabolized by several CYP450 isoenzymes (3A4, 2B6, 2C19, 2C9). However, interactions with inhibitors or inducers have not been observed. Interactions are possible with drugs that increase the risk of bleeding, for example, vitamin K antagonists and NSAIDs. Opioids may affect the absorption of prasugrel.
Adverse effects
The most common adverse effects include bleeding.